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Oral controlled release dosage form

  • US 8,252,327 B2
  • Filed: 07/11/2011
  • Issued: 08/28/2012
  • Est. Priority Date: 12/09/2002
  • Status: Expired due to Fees
First Claim
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1. A controlled release methylphenidate tablet consisting of:

  • (A) an immediate release methylphenidate coating consisting of;

    (a) 30-60 weight percent based upon the total weight of the immediate release coating of methylphenidate or a pharmaceutically acceptable salt or isomer thereof;

    (b) 40-70 weight percent based upon the total weight of the immediate release coating of a binder; and

    (c) 0.005-5 weight percent based upon the total weight of the immediate release coating of an organic acid;

    (B) a controlled release methylphenidate core tablet consisting of;

    (a) a compressed mixture consisting of;

    (i) 5-40 weight percent based upon the total weight of the compressed mixture of methylphenidate or a pharmaceutically acceptable salt or isomer thereof;

    (ii) 3-40 weight percent based upon the total weight of the compressed mixture of a hydrogel polymer;

    (iii) 25-90 weight percent based upon the total weight of the compressed mixture of a diluent; and

    (iv) optionally a lubricant; and

    (b) an enteric coating surrounding the core tablet consisting of;

    (i) 10-70 weight percent based upon the total weight of the enteric coating of a methacrylic acid copolymer;

    (ii) 1-5 weight percent based upon the total weight of the enteric coating of a plasticizer;

    (iii) an anti-sticking agent; and

    (iv) optionally a surfactant; and

    (C) optionally an aesthetic coating;

    wherein the controlled release methylphenidate tablet exhibits the following dissolution profile when tested in a United States Pharmacopeia type 2 (paddle) apparatus at 50 rpms in 900 ml of phosphate buffer with a pH of 7.5 and at 37°

    C.;

    1-35% of the methylphenidate is released after 1 hour;

    5-40% of the methylphenidate is released after 2 hours; and

    not less than 70% is release after 10 hours; and

    when administered to humans exhibits a plasma peak for the immediate release layer (Tmax1) between 1 and 5 hours, a plasma peak for the controlled release core (Tmax2) between 4 and 12 hours, and a plasma trough (Tmin) between 2 and 7 hours in between the two peak plasma levels; and

    wherein the immediate release methylphenidate coating (A) is applied to the enteric coating surrounding the core tablet.

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